CA2902755C - Derives de 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine en tant que modulateurs de l'activite kinase - Google Patents

Derives de 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine en tant que modulateurs de l'activite kinase Download PDF

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Publication number
CA2902755C
CA2902755C CA2902755A CA2902755A CA2902755C CA 2902755 C CA2902755 C CA 2902755C CA 2902755 A CA2902755 A CA 2902755A CA 2902755 A CA2902755 A CA 2902755A CA 2902755 C CA2902755 C CA 2902755C
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Canada
Prior art keywords
fluoro
imidazol
ethyl
phenyl
piperidin
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Active
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CA2902755A
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English (en)
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CA2902755A1 (fr
Inventor
Ruoxi Lan
Xiaoling Chen
Yufang Xiao
Bayard R. Huck
Andreas Goutopoulos
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Merck Patent GmbH
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Merck Patent GmbH
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

L'invention concerne de nouveaux amides hétérocycliques selon la formule (I), leur fabrication et leur utilisation pour le traitement de maladies hyperprolifératives, telles que le cancer. Formule (I).
CA2902755A 2013-03-11 2014-03-10 Derives de 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine en tant que modulateurs de l'activite kinase Active CA2902755C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361776440P 2013-03-11 2013-03-11
US61/776,440 2013-03-11
PCT/US2014/022479 WO2014143612A1 (fr) 2013-03-11 2014-03-10 Dérivés de 6-[4-(1 h-imidazol-2-yl)pipéridin-1 -yl]pyrimidin-4-amine en tant que modulateurs de l'activité kinase

Publications (2)

Publication Number Publication Date
CA2902755A1 CA2902755A1 (fr) 2014-09-18
CA2902755C true CA2902755C (fr) 2021-02-16

Family

ID=50440836

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2902755A Active CA2902755C (fr) 2013-03-11 2014-03-10 Derives de 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine en tant que modulateurs de l'activite kinase

Country Status (17)

Country Link
US (2) US9458134B2 (fr)
EP (1) EP2970201B1 (fr)
JP (1) JP6483656B2 (fr)
KR (1) KR20150124957A (fr)
CN (1) CN105209454A (fr)
AR (1) AR095202A1 (fr)
AU (1) AU2014228385B2 (fr)
BR (1) BR112015021324A2 (fr)
CA (1) CA2902755C (fr)
ES (1) ES2746756T3 (fr)
HK (1) HK1218756A1 (fr)
IL (1) IL240875B (fr)
MX (1) MX370448B (fr)
RU (1) RU2674261C2 (fr)
SG (2) SG11201505999VA (fr)
WO (1) WO2014143612A1 (fr)
ZA (1) ZA201505749B (fr)

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MX370448B (es) * 2013-03-11 2019-12-13 Merck Patent Gmbh Derivados de 6- [4- (1h-imidazol-2-il) piperidin-1-il] pirimidin-4-amina como moduladores de la actividad de cinasa.
US9434714B2 (en) * 2014-02-11 2016-09-06 Merck Patent Gmbh Pyrimidine imidazole amines as modulators of kinase activity
ES2768900T3 (es) * 2014-04-03 2020-06-24 Merck Patent Gmbh Combinaciones de agentes terapéuticos contra cáncer
TWI732187B (zh) * 2016-05-20 2021-07-01 日商大鵬藥品工業股份有限公司 新穎5H-吡咯并[2, 3-d]嘧啶-6(7H)-酮衍生物
CN110922354B (zh) * 2019-12-12 2023-05-02 丽水绿氟科技有限公司 一种1-r-3-氟哌啶-4-羧酸的化学拆分制备方法及其产物
US11866421B2 (en) 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment

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US7754722B2 (en) * 2002-09-20 2010-07-13 Merck Serono Sa Piperazine derivatives and methods of use
CA2522595A1 (fr) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions utiles en tant qu'inhibiteurs de proteines kinases
WO2005033086A1 (fr) 2003-09-30 2005-04-14 Irm Llc Composes et compositions inhibant les proteines-kinases
CA2541989C (fr) 2003-10-24 2013-10-01 Exelixis, Inc. Modulateurs des p70s6 kinases et procede d'utilisation
KR20060117329A (ko) 2003-11-21 2006-11-16 노파르티스 아게 단백질 키나제 저해제로서의 1ｈ-이미다조퀴놀린 유도체
TR200808208T1 (tr) 2003-12-09 2008-12-22 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Bir immün tepkinin bastırılması veya proliferatif bir hastalığın tedavisi
GB0403606D0 (en) * 2004-02-18 2004-03-24 Novartis Ag Organic compounds
CA2563699C (fr) 2004-04-23 2014-03-25 Exelixis, Inc. Modulateurs de kinase et methode d'utilisation
JP5274842B2 (ja) 2004-12-28 2013-08-28 エグゼリクシス， インコーポレイテッド 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
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UA99284C2 (ru) * 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
BRPI0921840A2 (pt) * 2008-11-11 2018-10-09 Lilly Co Eli produto compreendendo o composto inibidor de p70 s6 quinase e inibidor de mtor, composto inibidor de p70 s6 quinase e uso do mesmo
BRPI0921888A2 (pt) * 2008-11-11 2015-12-29 Lilly Co Eli terapia de combinação de inibidor de egfr inibidor da p70 s6 quinase
AR074072A1 (es) 2008-11-11 2010-12-22 Lilly Co Eli Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme
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UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
CA2803387C (fr) 2010-07-29 2017-12-05 Bayard R. Huck Carboxamides azaheterocycliques d'amines cycliques
LT2643313T (lt) 2010-11-24 2016-10-25 Merck Patent Gmbh Chinazolino karboksamido azetidinai
DK2718270T3 (da) * 2011-06-10 2022-08-01 Merck Patent Gmbh Sammensætninger og fremgangsmåder til fremstillingen af pyrimidin- og pyridinforbindelser med btk-hæmmende aktivitet
EP3263568B1 (fr) * 2011-07-18 2021-08-25 Merck Patent GmbH Benzamides
CN104080782B (zh) * 2011-09-12 2016-06-01 默克专利有限公司 用作激酶活性调节剂的咪唑胺
KR101992505B1 (ko) * 2011-09-12 2019-06-24 메르크 파텐트 게엠베하 키나아제 활성의 조절제로서 용도를 위한 아미노피리미딘 유도체
LT2794571T (lt) * 2011-12-22 2017-02-10 Merck Patent Gmbh Naujieji heterocikliniai karboksamidai kaip kinazės aktyvumo moduliatoriai
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MX370448B (es) * 2013-03-11 2019-12-13 Merck Patent Gmbh Derivados de 6- [4- (1h-imidazol-2-il) piperidin-1-il] pirimidin-4-amina como moduladores de la actividad de cinasa.
US9434714B2 (en) * 2014-02-11 2016-09-06 Merck Patent Gmbh Pyrimidine imidazole amines as modulators of kinase activity
WO2015134536A1 (fr) * 2014-03-04 2015-09-11 Plexxikon Inc. Composés et méthodes de modulation des kinases, et leurs indications

Also Published As

Publication number Publication date
CN105209454A (zh) 2015-12-30
SG11201505999VA (en) 2015-08-28
EP2970201A1 (fr) 2016-01-20
MX370448B (es) 2019-12-13
US20160016936A1 (en) 2016-01-21
IL240875A0 (en) 2015-10-29
US9867826B2 (en) 2018-01-16
AR095202A1 (es) 2015-09-30
JP2016512509A (ja) 2016-04-28
ES2746756T3 (es) 2020-03-06
RU2674261C2 (ru) 2018-12-06
ZA201505749B (en) 2017-01-25
WO2014143612A1 (fr) 2014-09-18
RU2015143160A (ru) 2017-04-18
AU2014228385A1 (en) 2015-08-20
HK1218756A1 (zh) 2017-03-10
US9458134B2 (en) 2016-10-04
BR112015021324A2 (pt) 2017-07-18
KR20150124957A (ko) 2015-11-06
IL240875B (en) 2020-08-31
SG10201900954SA (en) 2019-02-27
AU2014228385B2 (en) 2018-08-09
RU2015143160A3 (fr) 2018-03-01
MX2015011660A (es) 2015-12-16
JP6483656B2 (ja) 2019-03-13
CA2902755A1 (fr) 2014-09-18
US20160361316A1 (en) 2016-12-15
EP2970201B1 (fr) 2019-06-19

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